Adaptaquin-d₄

Adaptaquin-d₄ is intended for use as an internal standard for the quantification of adaptaquin (Item No. 19720) by GC- or LC-MS. Adaptaquin is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC₅₀ = 2 µM).¹ It stabilizes HIF-1α protein and induces expression of the HIF-1-regulated genes EPO and VEGF in SH-SY5Y human neuroblastoma cells. Adaptaquin protects against cell death induced by glutathione depletion in rat primary cortical neurons (IC₅₀ = 0.25 μM) and reduces glutamate-induced cell death in HT22 cells.^1,2 In vivo, adaptaquin (30 mg/kg) increases pellet retrieval in the single-pellet reaching task in a rat autologous striatal blood infusion model of intracerebral hemorrhage and normalizes preference for ipsilateral turns in a mouse model of striatal hemorrhage.³

WARNING This product is not for human or veterinary use.

1. Smirnova, N.A., Rakhman, I., Moroz, N., et al. Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation. Chem. Biol. 17(4), 380-391 (2010).

2. Neitemeier, S., Dolga, A.M., Honrath, B., et al. Inhibition of HIF-prolyl-4-hydroxylases prevents mitochondrial impairment and cell death in a model of neuronal oxytosis. Cell Death Dis. 7, e2214 (2016).

3. Karuppagounder, S.S., Alim, I., Khim, S.J., et al. Therapeutic targeting of oxygen-sensing prolyl hydroxylases abrogates ATF4-dependent neuronal death and improves outcomes after brain hemorrhage in several rodent models. Sci. Transl. Med. 8(328), (2016).